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Psychopharmacology > Pharmokinetics / pharmacodynamics > Flashcards

Pharmokinetics / pharmacodynamics Flashcards

1
Q

Partition coefficient (lipid/water)

A

dissolve drug in water, add equal volume fat, see where drug separates

[oil] / [water] = coefficient

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2
Q

Aspirin ionization

A

Gets deionized in the stomach (carboxyl group)

Reionized in intestine, then can’t leave

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3
Q

How long for a drug to be available all over the body once in the blood?

A

~120 sec

Mana said ‘within a minute’

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4
Q

Pharmacodynamics

A

Study of biochemical and physical effects of drugs

binding to effector proteins

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5
Q

What is depot binding?

A

When drugs bind to other proteins / tissues (e.g. fat, bone marrow, etc)

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6
Q

If a drug binds to bone marrow, what happens in terms of concentration, etc?

A

Drug stays in the body longer

Less drug at the intended site of action

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7
Q

How / where are most drugs inactivated?

A

The liver

Broken down / altered by enzymes

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8
Q

Is glucose a drug?

A

No.

Drug = non-nutritive chemical that alters physiology

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9
Q

If you alter the sympathetic nervous system but not the CNS with a chemical, is that a psychoactive drug?

A

No. Chemicals must get through the BBB and get into the CNS to be considered a drug.

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10
Q

What is pharmacokinetics?

A

How drugs move around.

How they’re administered, where they go once you administer them, how they’re metabolized, how they leave the body

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11
Q

pharmacokinetic binding

A

The exact way in which a drug attaches to a receptor, pump, enzyme, etc.

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12
Q

How are drugs inactivated in metabolism?

A

increase polarity of drug so that it can’t go through stuff

Lots of other stuff

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13
Q

What is the most common route of drug administration?

What are the advantages / disadvantages?

A

Oral: safe, don’t need help

Problems: all kinds of things can change how fast you absorb it. Hard to predict

First-pass metabolism

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14
Q

What is the vomiting area of the medulla called?

How does it determine vomiting?

A

area postrema
Area in the medulla with no BBB
Samples blood to determine if you should throw up

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15
Q

What are some other ways to get drugs in your body?

A

ICV (intraventricularly): directly into brain
IV (intravenous): into blood
IM (instramuscularly): Localized at injection site.

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16
Q

How fast are the effects of inhalation?

A

Almost immediate - heavily vascularized, thin membranes in the lungs

Every molecule has the chance to go to brain before liver

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17
Q

What is first-pass metabolism?

A

Drug gets metabolized in the liver for excretion before it does other stuff

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18
Q

What is the ‘vehicle’ for a drug?

A

The medium through which it’s delivered

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19
Q

Why is rectal administration useful?

A

Lower third of digestive system doesn’t suffer from first-pass problems (doesn’t pass through liver)

Huge absorptive surface there

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20
Q

What is the route for first-pass metabolism?

A

Anything that goes through liver (up to 20-30% of drug inactivated before it gets to brain)

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21
Q

How much total drug movement is there for aspirin in stomach vs. small intestine?

A

More in small intestine, BECAUSE of absorptive surface!

With same amount of absorptive surface, stomach would be better

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22
Q

What does a drug need to get into the CNS?

A

Small, lipid-soluble, or transported

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23
Q

What are platelets? What do they relate to?

A

Proteins found in blood

Depot binding - psychoactive drugs can bind to them instead of go into CNS

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24
Q

What do liver enzymes do?

A

Break the drug down (change it structurally so that it can’t bind)

Normally make more water soluble

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25
Q

What are metabolites?

Active metabolites?

A

Products of a liver enzyme. Has been chemically changed somehow

Active: Exert psychoactive effects after becoming metabolites

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26
Q

What happens in phase II metabolism?

A

You add stuff - change structure so that it can’t bind to stuff. New functional groups

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27
Q

What happens in Phase I metabolism?

A

Oxidation / reduction

Structure isn’t changed though (as in, new functional groups don’t get added)

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28
Q

Where are polar drug species excreted?

A

Urine (‘renal elimination’)

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29
Q

Where are nonpolar drug species excreted?

A

Feces (‘biliary elimination’)

30
Q

What is cross-tolerance?

A

e.g. history of cigarette smoking causes ethanol tolerance

The same enzyme metabolizes two drugs, so taking one drug helps with metabolism of the other

31
Q

What is zero-order kinetics?

A

Rate of metabolism is constant / linear

32
Q

What is first-order kinetics?

A

Rate of metabolism greater with more plasma levels - exponential decrease

33
Q

What is the half-life?

A

Time it takes for drug to eliminate to 1/2 of its peak plasma level

34
Q

What does the half-life look like with zero-order kinetics?

A

Half-life decreases with decreasing concentration

35
Q

What does the half-life look like with first order kinetics?

A

Length of half-life is constant

36
Q

Specific vs. nonspecific drug effects

A

Specific: effects based on interactions of a drug with target tissue

Nonspecific: based on characteristics of the individual taking the drug, not on the drug’s interactions with target tissue (e.g. mood at the time, diet, etc)

37
Q

Example of nonspecific drug effect?

A

e.g. placebo

38
Q

What are enteral methods of drug administration?

A

Use the gastrointestinal tract to get agents in the body

39
Q

What kinds of enteral administration are there?

A

oral, through rectal cavities

40
Q

What is the opposite of enteral administration?

A

parenteral

e.g. injection, pulmonary, topical administration

41
Q

topical administration

A

administration to body surface

42
Q

What are four effects of depot binding?

A
  • Drugs stay in tissue longer
  • Drugs that compete for depots could be displaced
  • onset of action could be delayed
  • Depots could be responsible for termination e.g they go to CNS first, but then depots change blood/brain concentration difference and cause them to leave cns faster
43
Q

What are microsomal enzymes and where are they found?

A

Liver enzymes that metabolize psychoactive drugs

Found in smooth ER of liver cells

44
Q

What class of microsomal enzyme is responsible for metabolizing most psychoactive drugs?

A

Cytochrome P450 (CYP450)

45
Q

What is Kd in relation to pharmacodynamics?

A

Affinity of drug for receptor.

Kd = [drug][receptors] / [drug + receptors]

Drug + target –> Drug-target complex

46
Q

If you have a higher Kd, what happens to the drug’s affinity for a receptor?

A

Drug has less affinity for receptor (higher concentration of drug/receptor individually)

47
Q

What is the term for how well a ligand activates a receptor / produces a functional response?

A

intrinsic activity

48
Q

What is the magnitude of a drug’s effects called?

A

Potency

49
Q

What makes a drug more potent?

A

affinity and intrinsic activity

50
Q

What is an inverse agonist? How is it different than an antagonist?

A

An inverse agonist actively creates a negative response (has effects by itself)

An antagonist simply prevents a positive response (can’t have an effect by itself)

51
Q

What is the drug dose generally described in terms of?

A

Weight of drug / weight of recipient

in a given volume of vehicle

52
Q

What is the ED50 of a dose response curve?

A

The dose at which 50% of people taking the drug have the response that specific curve is measuring

53
Q

What two things do you need on a good dose response curve?

A

One dose at 0, so you know where there’s no effect

A second dose past the asymptote, so that you know there is an asymptote

54
Q

What is the therapeutic window for a drug defined as?

A

You’re past the ED10 of the therapeutic effect

You’re before the ED10 of the toxic effect

55
Q

What drugs make up the stimulants?

A

Amphetamine
Cocaine
Nicotine

56
Q

What drugs make up the depressants?

A

Barbituates

Alcohol

57
Q

What drugs make up the analgeisics?

A

Morphine

Codeins

58
Q

What drugs make up the hallucinogens?

A

Mescaline
LSD
Psilocybin

59
Q

What drugs make up the psychotherapeutics?

A

Prozac

Thorazine

60
Q

Synergistic drug effects

A

Both drugs together cause a greater overall effect

Additive effects or potentiation

61
Q

Antagonistic drug effects

A

Both drugs together cause decreased effect

62
Q

Drug code names

A

e.g. Ro 5-2807

5 = general structure
Ro = company
2807 = iteration of it
63
Q

decongestant

A

Shrink swollen blood vessels

64
Q

What is a pharmacological activity classification?

A

Classify drugs according to primary pharmacological activity

But there can be multiple effects

65
Q

What effect of a compound is used mainly to classify them?

A

The compound’s therapeutic use

66
Q

Do you want a high or low TI?

A

High
More TI = you can take more of the drug without worrying about a bad side effect

Safer drug

67
Q

What is TI?

A

Therapeutic index

Ratio of LD50 to ED50 (lethal dose to effective dose)

68
Q

What is oral administration?

A

Take by mouth

69
Q

What is intravenous administration?

A

Put in veins (depleted O2)

70
Q

What is intraperitoneal administration?

A

Put drugs into the body cavity

71
Q

What is subcutaneous administration?

A

Put drugs directly under skin

72
Q

What is intramuscular injection?

A

Into the muscles

Psychopharmacology (12 decks)

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